Pharmaceutical composition

Abstract

A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]-heptanedicarboxylmide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied.

The invention claimed is: 
     
       1. An oral preparation comprising 20 to 120 mg of N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1′R,2′S,3′R,4′S)-2,3-bicyclo[2,2,1]heptanedicarboxylmide hydrochloride (lurasidone) of formula (1): 
       
         
           
           
               
               
           
         
       
       a pregelatinized starch, a water-soluble excipient, a water-soluble polymer binder, a disintegrant, and a lubricant, wherein the content of lurasidone in the preparation is 20 to 45% (wt/wt), and the content of the pregelatinized starch in the preparation is 20 to 30% (wt/wt). 
     
     
       2. The oral preparation of  claim 1 , wherein the water-soluble excipient is mannitol or lactose, and the content of water-soluble excipient in the preparation is 40 to 60% (wt/wt). 
     
     
       3. The oral preparation of  claim 2 , wherein the water-soluble excipient is mannitol. 
     
     
       4. The oral preparation of  claim 3 , wherein the water-soluble binder is hydroxypropyl methylcellulose, polyvinyl alcohol, polyvinylpyrrolidine or hydroxypropylcellulose, and the content of water-soluble binder in the preparation is 1 to 5% (wt/wt). 
     
     
       5. The oral preparation of  claim 4 , wherein the water-soluble binder is hydroxypropyl methylcellulose. 
     
     
       6. The oral preparation of  claim 5 , wherein the disintegrant is corn starch, crystalline cellulose, low substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, carboxymethyl starch sodium, or crospovidone, and the content of the disintegrant in the preparation is 0.5 to 5% (wt/wt). 
     
     
       7. The oral preparation of  claim 6 , wherein the disintegrant is croscarmellose sodium. 
     
     
       8. The oral preparation of  claim 7 , wherein the lubricant is magnesium stearate, talc, polyethylene glycol, silica or hydrogenated vegetable oil, and content of the lubricant in the preparation is 1.0 to 1.43% (wt/wt). 
     
     
       9. The oral preparation of  claim 8 , wherein the lubricant is magnesium stearate. 
     
     
       10. The oral preparation of  claim 9 , wherein the content of lurasidone is 20 mg. 
     
     
       11. The oral preparation of  claim 9 , wherein the content of lurasidone is 40 mg. 
     
     
       12. The oral preparation of  claim 9 , wherein the content of lurasidone is 80 mg. 
     
     
       13. The oral preparation of  claim 9 , wherein the content of lurasidone is 120 mg. 
     
     
       14. The oral preparation of  claim 1 , wherein the oral preparation is a tablet.